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MACROLIDE COMPOSITIONS HAVING IMPROVED TASTE AND STABILITY
专利权人:
发明人:
申请号:
EP09718249.7
公开号:
EP2259773B1
申请日:
2009.03.05
申请国别(地区):
EP
年份:
2013
代理人:
摘要:
The invention provides an aqueous pharmaceutical composition for administration as an aerosol to the respiratory tract, nose or oropharyngeal region comprising (i) a macrolide having a poor taste and poor chemical stability in aqueous solution (ii) at least one salt selected from the group consisting of sodium gluconate, sodium aspartate, sodium acetate, sodium lactate, sodium succinate, sodium maleate, magnesium gluconate, magnesium aspartate, magnesium citrate, magnesium acetate, magnesium lactate, magnesium succinate, and magnesium maleate or mixtures thereof and (iii) a taste-masking agent different from said salt wherein (a) the concentration of said macrolide in the composition is in the range of about 0.25 wt.-% to about 15 wt.-% (b) the molar ratio of said macrolide : said salt is in the range from about 1 : 0.5 to about 1 : 100 (c) the pH of the composition is in the range of about 3 to 9 and (d) the osmolality of the composition is in the range of about 150 mOsmol/kg to about 1500 mOsmo I/kg. The invention further provides a method of generating an aerosol, preferably by means of a nebuliser, which uses such an aqueous pharmaceutical composition. The macrolide may be used alone or in combination with other drugs. The composition is suitable to treat inflammatory disorders and/or infections of the respiratory tract. It has an improved taste and stability.Linvention porte sur une composition pharmaceutique aqueuse à administrer sous forme daérosol au tractus respiratoire, au nez ou à la région oropharyngée, comprenant (i) un macrolide ayant un goût médiocre et une stabilité chimique médiocre en solution aqueuse (ii) au moins un sel choisi dans le groupe constitué par le gluconate de sodium, laspartate de sodium, lacétate de sodium, le lactate de sodium, le succinate de sodium, le maléate de sodium, le gluconate de magnésium, laspartate de magnésium, le citrate de magnésium, lacétate de magnésium, le lactate de magnésium, le succinate de magnésium et le malé
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中国工程科技知识中心
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